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UC 112 IAP inhibitor

Catalog No.B7790
Size Price Stock Qty
10mg
$183.00
In stock
50mg
$771.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

UC 112

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Chemical Properties

Cas No. 383392-66-3 SDF Download SDF
Chemical Name 5-((benzyloxy)methyl)-7-(pyrrolidin-1-ylmethyl)quinolin-8-ol
Canonical SMILES OC1=C2C(C=CC=N2)=C(COCC3=CC=CC=C3)C=C1CN4CCCC4
Formula C22H24N2O2 M.Wt 348.44
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical Appearance White solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

UC-112[5-((benzyloxy)methyl)-7-(pyrrolidin-1-ylmethyl)quinolin-8-ol], is inhibitor of inhibitor of apoptosis protein (IAP).[1]

Inhibitor of apoptosis protein (IAP) family is overexpressed in most human cancer cells, but nearly isn’t expressed in adult differentiated tissues. Inhibitor of apoptosis (IAP) proteins are widely considered as promising drug-resistant tumors drug targets. [1,2]

UC-112 strongly activates caspase-3/7 and caspase-9 activities, and selectively reduce surviving level at a concentration as low as 1 mM. Coincubation of UC-112 with a known proteasome inhibitor Z-Leu-Leu-Leu-CHO (MG-132) rescued survivin inhibition. As a single agent, UC-112 strongly inhibits tumor growth and reduces both X chromosomelinked IAP and survivin levels in an A375 human melanoma xenograft model in vivo.[1]

UC-112 inhibits tumor cell growth in several cancer cell lines in vitro and suppresses melanoma tumor growth in vivo. Mechanistic studies indicated that UC-112 selectively inhibits survivin expression and induces strong cancer cell apoptosis. UC-112 could efficiently inhibit tumor cell proliferation by down regulating the level of IAPs, especially survivin protein.[1,2]

References:
[1] Wang J, Li W.  Discovery of novel second mitochondria-derived activator of caspase mimetics as selective inhibitor of apoptosis protein inhibitors. J Pharmacol Exp Ther. 2014 May;349(2):319-29.
[2] Xiao M, Wang J, Lin Z, etal. , Design, Synthesis and Structure-Activity Relationship Studies of Novel Survivin Inhibitors with Potent Anti-Proliferative Properties. PLoS One. 2015 Jun 12;10(6):e0129807.